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Cytochrome P450 2C19 (CYP2C19) Inhibitor Screening Kit (Fluorometric) (CAT#: CB-P239-K) Datasheet

Product Type
Cytochrome P450 2C19 (CYP2C19, EC is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolizing enzymes. CYP is the membrane-bound hemoglobin responsible for the phase I biotransformation reaction, in which lipophilic drugs and other heterogeneous biological compounds are converted into more hydrophilic products to promote human excretion. CYP2C19 is mainly expressed in liver and intestinal tissues, and catalyzes the oxidation of neutral or weakly alkaline lipophilic molecules with 2-3 hydrogen bond donor/acceptor sites. The isoforms of the CYP2C subfamily are responsible for nearly 20% of the metabolism of all small molecule drugs commonly used in humans. The polymorphism of the human CYP2C19 gene is related to clinical drug/drug interactions involving a wide range of prescription drugs, including proton pump inhibitors, antiplatelet drugs, and anticonvulsants. In addition, for drugs whose pharmacological activity needs to be metabolized from the prodrug form (such as the antithrombotic drug clopidogrel), CYP2C19 inhibition or allele deficiency can lead to reduced drug efficacy. Cre
100 assays

Figure 1 3-cyano-7-hydroxycoumarin (3-CHC) standard curve.

Figure 2 Reaction kinetics of recombinant human CYP2C19 enzyme at 37°C in the presence and absence of the indicated CYP2C19 inhibitors.

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